- Synthesis and evaluation of antiepileptic activity of newly designed coumarin-sulfonamide hybrids
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The combination of different heterocyclic rings to form a multifunctional compound is a new approach to get the potent and selective compounds, which can act as antiepileptic drugs. In this study we designed and synthesized the hybrid of the coumarin ring with sulfonamide moiety. Coumarin sulfonamide hybrids (CS1-CS7) were synthesized by Knoevenagel condensation of methyl anilinosulfonyl acetate with substituted salicyaldehyde in the presence of catalytic base. The synthesized hybrid compounds were characterized by means of mass, 1H & 13C NMR and FTIR spectroscopy, moreover antiepileptic activity was screened through seizure model of epilepsy using pentylenetetrazole and maximal electroshock. According to results, compound CS-2 remained to be highest potent and presented significant protection at 60 mg/kg in both the seizure models. Furthermore, compound CS-2 was also evaluated for biochemical and a histopathological study in which no significant results were obtained. In addition to former activities, compound CS-2 was also examined for liver toxicity.
- Dhiman, Neerupma,Gupta, Arti,Kumar, Sandeep,Mallikarjun, B. P.,Sharma, Archana,Singh, Vijay Kumar
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p. 3108 - 3114
(2021/12/14)
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- Synthesis and biological evaluation of heteroaryl styryl sulfone derivatives as anticancer agents
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Herein we disclose a series of novel heteroaryl styryl sulfone derivatives as potential anticancer agents. Structure-activity relationships of these newly synthesised compounds were explored with respect to the significance of the position and number of nitrogen atom of the heteroaryl ring for anti-proliferative activity in human cancer cell lines. A lead compound 14f was tested against a panel of cancerous and untransformed cell lines, and found to be highly potent against cancer cells with minimal toxicity in the untransformed cells. Further mechanistic studies uncovered that 14f caused cell-cycle arrest at the G2/M phase and induced apoptosis by targeting CDC25C and Mcl-1 proteins in A2780 ovarian cells.
- Long, Yi,Yu, Mingfeng,Li, Peng,Islam, Saiful,Goh, Aik Wye,Kumarasiri, Malika,Wang, Shudong
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p. 5674 - 5678
(2016/11/25)
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- Design, synthesis, and biological evaluation of (E)-N-Aryl-2- arylethenesulfonamide analogues as potent and orally bioavailable microtubule-targeted anticancer agents
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A series of novel (E)-N-aryl-2-arylethenesulfonamides (6) were synthesized and evaluated for their anticancer activity. Some of the compounds in this series showed potent cytotoxicity against a wide spectrum of cancer cell-lines (IC50 values ranging from 5 to 10 nM) including all drug resistant cell-lines. Nude mice xenograft assays with compound (E)-N-(3-amino-4- methoxyphenyl)-2-(2′,4′,6′-trimethoxyphenyl)ethenesulfonamide (6t) showed dramatic reduction in tumor size, indicating their in vivo potential as anticancer agents. A preliminary drug development study with compound 6t is predicted to have increased blood-brain barrier permeability relative to many clinically used antimitotic agents. Mechanistic studies indicate that 6t and some other analogues disrupted microtubule formation, formation of mitotic spindles, and arrest of cells in mitotic phase. Compound 6t inhibited purified tubulin polymerization in vitro and in vivo and circumvented drug resistance mediated by P-glycoprotein. Compound 6t specifically competed with colchicine binding to tubulin and with similar avidity as podophylltoxin, indicating its binding site on tubulin.
- Reddy, M. V. Ramana,Mallireddigari, Muralidhar R.,Pallela, Venkat R.,Cosenza, Stephen C.,Billa, Vinay K.,Akula, Balaiah,Subbaiah, D. R. C. Venkata,Bharathi, E. Vijaya,Padgaonkar, Amol,Lv, Hua,Gallo, James M.,Reddy, E. Premkumar
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p. 5562 - 5586
(2013/07/26)
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- Synthesis of new coumarin 3-(N-aryl) sulfonamides and their anticancer activity
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Synthesis of coumarin 3-(N-aryl) sulfonamides was accomplished either by Knoevenagel condensation of anilinosulfonylacetic acids with suitable salicylaldehydes or by the reaction of methyl anilinosulfonylacetates with substituted salicylaldehydes in presence of a catalytic amount of a base. All the compounds tested for antiproliferative activity in different cancer cell lines have shown GI50 values less than 100μM.
- Reddy, Natala Srinivasa,Mallireddigari, Muralidhar Reddy,Cosenza, Stephen,Gumireddy, Kiranmai,Bell, Stanley C.,Reddy, E. Premkumar,Reddy, M.V. Ramana
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p. 4093 - 4097
(2007/10/03)
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- Synthesis and Biological Activity of Some New 2--N-arylsulphonamides and 1-sulphonyl Heterocycles
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Several new 2--N-arylsulphonamides (10-12) and 1-2-(5-nitro-2-furyl- and 5-nitro-2-thienyl)vinyl sulphonyl heterocycles (13-16) have been synthesized and evaluated for various biological activities.Three com
- Shridhar, D. R.,Sastry, C. V. Reddy,Lal, K. B.,Marwah, A. K.,Reddi, G. S.,et al.
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p. 234 - 237
(2007/10/02)
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